Improvement of Aqueous Solubility of Lapatinib-derived Analogs: Identification of a Quinolinimine as a Lead for Human African Trypanosomiasis Drug Development

Lapatinib, an approved EGFR inhibitor, was explored as a starting point for the synthesis of new hits against Trypanosoma brucei, the causative agent of human African trypanosomiasis (HAT). Previous work culminated in 1 (NEU-1953), which was part of a series typically associated with poor aqueous so...

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Publié dans:J Med Chem
Auteurs principaux: Bachovchin, Kelly A., Sharma, Amrita, Bag, Seema, Klug, Dana M., Schneider, Katherine M., Singh, Baljinder, Jalani, Hitesh B., Buskes, Melissa J., Mehta, Naimee, Tanghe, Scott, Momper, Jeremiah D., Sciotti, Richard J., Rodriguez, Ana, Mensa-Wilmot, Kojo, Pollastri, Michael P., Ferrins, Lori
Format: Artigo
Langue:Inglês
Publié: 2019
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Article
Accès en ligne:https://ncbi.nlm.nih.gov/pmc/articles/PMC6556231/
https://ncbi.nlm.nih.gov/pubmed/30565932
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/acs.jmedchem.8b01365
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